Dening Tahnee J, Rao Shasha, Thomas Nicky, Prestidge Clive A
School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, SA, 5001, Australia.
AAPS J. 2016 Jan;18(1):23-40. doi: 10.1208/s12248-015-9824-7. Epub 2015 Sep 9.
Lipid-based drug delivery systems (LBDDS) have gained significant attention in recent times, owing to their ability to overcome the challenges limiting the oral delivery of poorly water-soluble drugs. Despite the successful commercialization of several LBDDS products over the years, a large discrepancy exists between the number of poorly water-soluble drugs displaying suboptimal in vivo performances and the application of LBDDS to mitigate their various delivery challenges. Conventional LBDDS, including lipid solutions and suspensions, emulsions, and self-emulsifying formulations, suffer from various drawbacks limiting their widespread use and commercialization. Accordingly, solid-state LBDDS, fabricated by adsorbing LBDDS onto a chemically inert solid carrier material, have attracted substantial interest as a viable means of stabilizing LBDDS whilst eliminating some of the various limitations. This review describes the impact of solid carrier choice on LBDDS performance and highlights the importance of appropriate solid carrier material selection when designing hybrid solid-state LBDDS. Specifically, emphasis is placed on discussing the ability of the specific solid carrier to modulate drug release, control lipase action and lipid digestion, and enhance biopharmaceutical performance above the original liquid-state LBDDS. To encourage the interested reader to consider their solid carrier choice on a higher level, various novel materials with the potential for future use as solid carriers for LBDDS are described. This review is highly significant in guiding future research directions in the solid-state LBDDS field and fostering the translation of these delivery systems to the pharmaceutical marketplace.
基于脂质的药物递送系统(LBDDS)近年来受到了广泛关注,这是由于它们能够克服限制难溶性药物口服递送的挑战。尽管多年来有几种LBDDS产品成功实现了商业化,但在表现出次优体内性能的难溶性药物数量与应用LBDDS来缓解其各种递送挑战之间仍存在很大差异。传统的LBDDS,包括脂质溶液和混悬液、乳剂以及自乳化制剂,存在各种缺点,限制了它们的广泛使用和商业化。因此,通过将LBDDS吸附到化学惰性固体载体材料上制备的固态LBDDS,作为稳定LBDDS同时消除各种限制的一种可行手段,引起了极大的兴趣。本综述描述了固体载体选择对LBDDS性能的影响,并强调了在设计混合固态LBDDS时选择合适的固体载体材料的重要性。具体而言,重点讨论了特定固体载体调节药物释放、控制脂肪酶作用和脂质消化以及提高生物药剂学性能(高于原始液态LBDDS)的能力。为了鼓励感兴趣的读者从更高层面考虑他们对固体载体的选择,还描述了各种有潜力在未来用作LBDDS固体载体的新型材料。本综述对于指导固态LBDDS领域未来的研究方向以及促进这些递送系统向医药市场的转化具有重要意义。